Antiestrogenic activities of altenate-substituted polychlorinated dibenzofurans in MCF-7 human breast cancer cells

Gulan Sun, Stephen Safe

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

Purpose: 1,3,6,8-Substituted alkyl polychlorinated dibenzofurans (PCDFs), typified by 6-methyl-1,3,8-triCDF (MCDF), inhibit 17β-estradiol (E2)-induced responses in the rodent uterus and human breast cancer cells. The major purpose of the experiments reported here was to determine the structure-dependent antiestrogenic activities of several alternate-substituted (1,3,6,8- and 2,4,6,8-) PCDFs. Methods: The antiestrogenic activities were determined in MCF-7 human breast cancer cells using two assays, that is E2-induced cell proliferation and induction of chloramphenicol acetyl transferase (CAT) activity in cells transiently transfected with the E2-responsive Vit-CBT plasmid. Results: MCDF (10-5 M), 6-isopropyl-1,3,8-triCDF, 6-ethyl-1,3,8-triCDF, 3-isopropyl-6-methyl-1,8-diCDF, and 6-methyl-2,4,8-triCDF, inhibited both E2-induced cell proliferation and CAT activity in MCF-7 cells. All of the remaining ten congeners inhibited either E2-induced cell proliferation or CAT activity, but not both responses. Conclusions: The antiestrogenic activity of the alternate substituted PCDFs involves interactions between the aryl hydrocarbon and estrogen receptor signaling pathways. Although these compounds exhibited antiestrogenic activity in MCF-7 cells, the effects of individual congeners were response-specific, and there were no apparent structure-activity relationships.

Original languageEnglish (US)
Pages (from-to)239-244
Number of pages6
JournalCancer Chemotherapy and Pharmacology
Volume40
Issue number3
DOIs
StatePublished - 1997
Externally publishedYes

Keywords

  • Alternate-substituted PCDFs
  • Antiestrogens

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)

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